Modulators of Large-Conductance Calcium-Activated Potassium (BK) Channels as Potential Therapeutic Targets
Modulators of Large-Conductance Calcium-Activated Potassium (BK) Channels as Potential Therapeutic Targets
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大电导钙激活钾 (BK) 通道调节剂作为潜在治疗靶点
DOI：
10.2174/1381612802666220926184514
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发表时间：
1996
影响因子：
3.1
通讯作者：
V. Gribkoff
中科院分区：
文献类型：
--
作者：
John E. Starrett Jr.;S. Dworetzky;V. Gribkoff
BK通道是在许多组织中发现的大电导钙活化钾通道，包括肌细胞和神经元等可兴奋细胞。BK通道的高电导和对钙的依赖性表明，这些通道的调节可能对它们表达的组织有明显的影响。在过去的四年里，各种小分子和天然产物衍生的BK通道调节剂已经被描述。本文将重点介绍BK通道的打开剂和阻滞剂化合物及其治疗潜力，并介绍BK通道的生物物理学、药理学和分子生物学。
BK channels are large conductance calcium-activated potassium channels that are found in many tissues, including excitable cells such as myocytes and neurons. The high conductance and dependence on calcium of BK channels suggests that modulation of these channels may have a pronounced effect on tissues in which they are expressed. Within the past four years, a variety of small molecules and natural product-derived modulators of BK channels have been described. This review will focus on compounds which are openers and blockers of BK channels and their therapeutic potential, with introductory sections covering the biophysics, pharmacology and molecular biology of BK channels.